Effect of tissue penetration on AmBisome efficacy.
Effect of tissue penetration on AmBisome efficacy.
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组织渗透对 AmBisome 功效的影响。
DOI：
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发表时间：
2003
影响因子：
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通讯作者：
R. Proffitt
中科院分区：
文献类型：
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作者：
J. Adler;R. Proffitt
两性霉素B被重新配制成称为AmBisome的脂质体制剂（两性霉素B、氢化大豆磷脂酰胆碱、胆固醇和二肉豆蔻酰磷脂酰甘油），可以以比具有相同广谱活性的常规药物高15倍的剂量安全施用。剂量增加表明，随着网状内皮系统（RES）饱和和药物重新分布到非RES组织中，清除率呈非线性。该脂质体阿替霉素B制剂的功效似乎与肺、脑、肾、肝和脾中的组织渗透性改善以及这些靶组织中治疗药物水平的持续生物活性沿着有关。
Amphotericin B reformulated into the liposomal formulation known as AmBisome (amphotericin B, hydrogenated soy phosphatidylcholine, cholesterol and dimyristoyl phosphatidylglycerol) can be safely administered at dosages 15 times higher than the conventional drug with the same broad spectrum of activity. Increased doses demonstrate non-linear clearance with saturation of the reticuloendothelial system (RES) and redistribution of the drug into non-RES tissues. The efficacy of this liposomal amphotericin B formulation appears to be related both to improved tissue penetration in the lungs, brain, kidneys, liver and spleen along with sustained bioactivity of therapeutic drug levels in these target tissues.